1. Immunology/Inflammation
    PI3K/Akt/mTOR
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  2. COX
    Akt
    Apoptosis
  3. CAY10404

CAY10404 

Cat. No.: HY-121537 Purity: 99.79%
Handling Instructions

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

For research use only. We do not sell to patients.

CAY10404 Chemical Structure

CAY10404 Chemical Structure

CAS No. : 340267-36-9

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Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
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10 mg USD 180 In-stock
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25 mg USD 380 In-stock
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50 mg USD 650 In-stock
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100 mg USD 1050 In-stock
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Description

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[1][2][3].

IC50 & Target[1]

COX-2

1 nM (IC50)

COX-1

>500 μM (IC50)

Akt

 

In Vitro

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500 µM)[1].
CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100 µM[3].
CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells[3].
CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β[3].
CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460)
Concentration: 10-100 µM
Incubation Time: For 3 days
Result: Inhibited the growth of NSCLC cell lines in a concentration-dependent manner.

Apoptosis Analysis[3]

Cell Line: H460 cells
Concentration: 20, 50, 100 µM
Incubation Time: For 3 days
Result: Induced apoptosis.

Western Blot Analysis[3]

Cell Line: NSCLC cells (H358, H460)
Concentration: 80 µM
Incubation Time: For 3 days
Result: Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.
In Vivo

CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male C57Bl/6J mice weighing 24-30 g[2]
Dosage: 50 mg/kg
Administration: IP; daily; for 4 days
Result: Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α.
Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury.
Molecular Weight

367.34

Formula

C₁₇H₁₂F₃NO₃S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (272.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7223 mL 13.6114 mL 27.2227 mL
5 mM 0.5445 mL 2.7223 mL 5.4445 mL
10 mM 0.2722 mL 1.3611 mL 2.7223 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.81 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.79%

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CAY10404
Cat. No.:
HY-121537
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